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Generated: January 21, 2018

DrugPatentWatch Database Preview

Claims for Patent: 4,559,332

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Summary for Patent: 4,559,332
Title: 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
Abstract:Steroid compounds of the 20-spiroxane series and their analogues having an open ring E of the formula, ##STR1## in which --A--A-- represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R.sup.1 represents hydrogen, and R.sup.2 represents an .alpha.-oriented lower alkoxycarbonyl radical, or R.sup.1 and R.sup.2 together represent an .alpha.- or a .beta.-oriented methylene radical, --B--B-- represents the group --CH.sub.2 --CH.sub.2 -- or an .alpha.- or .beta.-oriented group ##STR2## X represents two hydrogen atoms or oxo, Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--, or Y.sup.1 represents hydroxy, and Y.sup.2 represents hydroxy, lower alkoxy or, if X represents H.sub.2, also lower alkanoyloxy, and salts of compounds in which X represents oxo and Y.sup.2 represents hydroxy, are distinguished as effective aldosterone-antagonists with minimal side-effects and, for that reason, are especially suitable for the treatment of all forms of hyperaldosteronism.
Inventor(s): Grob; Jurgen (Giebenach, CH), Kalvoda; Jaroslav (Binningen, CH)
Assignee: Ciba Geigy Corporation (Ardsley, NY)
Application Number:06/598,109
Patent Claims: 1. A steroid compound of the formula ##STR13## in which --A--A-- represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,

R.sup.1 represents hydrogen, and

R.sup.2 represents an .alpha.-oriented lower alkoxycarbonyl radical, or

R.sup.1 and R.sup.2 together represent an .alpha.- or a .beta.-oriented methylene radical,

--B--B-- represents the group --CH.sub.2 --CH.sub.2 -- or an .alpha.- or .beta.-oriented group ##STR14## X represents two hydrogen atoms or oxo, Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--, or

Y.sup.1 represents hydroxy, and

Y.sup.2 represents hydroxy, lower alkoxy or, if X represents H.sub.2, also lower alkanoyloxy,

and salts of compounds in which X represents oxo and Y.sup.2 represents hydroxy.

2. A compound according to claim 1, in which R.sup.2 represents methoxycarbonyl, ethoxycarbonyl or isopropoxycarbonyl.

3. A compound according to claim 1, in which R.sup.1 and R.sup.2 together represent a .beta.-oriented methylene radical.

4. A compound according to claim 1, in which --B--B-- represents the .beta.-oriented group ##STR15##

5. A compound according to claim 1, in which X represents oxo.

6. A compound according to claim 1, in which Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--.

7. A compound according to claim 1, in which R.sup.1 and R.sup.2 together represent a methylene group, X represents oxo and each of Y.sup.1 and Y.sup.2 represents hydroxy.

8. An alkali metal salt of a compound according to claim 7.

9. A potassium salt of a compound according to claim 7.

10. A compound according to claim 1, which is 9.alpha.,11.alpha.-epoxy-7.alpha.-methoxycarbonyl-20-spirox-4-ene-3,21-dio ne.

11. A compound according to claim 1, which is 9.alpha.,11.alpha.-epoxy-7.alpha.-isopropoxycarbonyl-20-spirox-4-ene-3,21- dione.

12. A compound according to claim 1, which is 9.alpha.,11.alpha.-epoxy-6.alpha.,7.alpha.-methylene-20-spirox-4-ene-3,21- dione.

13. A compound according to claim 1, which is 9.alpha.,11.alpha.-epoxy-6.beta.,7.beta.-methylene-20-spirox-4-ene-3,21-di one.

14. A pharmaceutical composition containing as active ingredient one of the compounds defined in claim 1.

15. A pharmaceutical composition containing an effective amount of an aldosterone-antagonistic compound according to claim 1, and at least one diuretic which is non-specific with regard to electrolytes and which increases diuresis by renal and by extrarenal action on tissue.

16. A therepeautic method for controlling hyperaldosteronism in humans and other warm-blooded animals, comprising the administration of an effective amount of a compound according to claim 1, in the presence or absence of a pharmaceutically acceptable carrier.

17. A therapeutic method for controlling hyperaldosteronism in humans and other warm blooded animals, comprising the simultaneous administration of an effective amount of a compound according to claim 1, together with at least one diuretic which is non-specific with regard to electrolytes and which increases diuresis by renal and by extrarenal action on tissue.

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Colorcon
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Harvard Business School
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Johnson and Johnson

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